多肽药物研究进展

The development in peptide-based drugs

人体内存在各种各样的天然多肽，它们参与调控各种生理功能，在临床应用上具有非常重要的开发价值。目前全球药物市场上有60～70个多肽药物，更多的多肽药物处在各级临床试验、临床前试验和实验室研究阶段。很多多肽药物以G蛋白偶联受体为靶点。传统的化学合成也仍然是开发多肽药物最主要的手段。然而，我们在多肽药物开发方面仍面临各种挑战，不仅要解决传统问题如不稳定，易降解，难穿越细胞膜，而且也要进一步降低生产成本，完善大批量生产工艺技术。尤其是多肽药物的口服生物利用度问题，一直是我们面临的最大的挑战和决定市场的关键因素。随着在现代技术及其它方面不断取得进展，多肽药物将具有更加广阔的前景。在新一代受体靶向药物研究中，多肽更被作为一种有效的药物载体，通过细胞表面受体将药物传递到特定细胞，达到提高特异性，减少副作用的目的。

Peptide drugs display such multiple and unique advantages as ready synthesis, quick optimization, fewer immune responses, less toxic side effects and rapid clearance. Signiifcant progress has been made in this ifeld. Currently, there are 60~70 peptide drugs in the global market, with many more under clinical and pre-clinical studies. Many of them are short, synthetic and long-acting peptides and mainly target G protein-coupled receptors （GPCRs）. These peptide drugs are mainly applied in treating cancers, cardiovascular diseases and metabolic disorders. However, such disadvantages as easy degradation, poor oral bioavailability and poor permeability hamper the clinical applications of these peptide drugs and limit their commercial markets. Despite of these challenges, it is believed that there is a promising future in peptide-based drug development due to the advances in peptide-associated technologies. In particular, it is a potential and critical approach for using peptides as drug delivery vehicles.